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US 2010/0168122 A1Published application
Xanthine derivatives as selective hm74a agonists
AssigneeSmithKline Beecham Corporation
InventorsRichard Jonathan Daniel Hatley, Andrew McMurtrie Mason, Ivan Leo Pinto
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Abstract
The present invention relates to compounds of formula (I) which are xanthine derivatives, processes for manufacture of said derivatives, pharmaceutical formulations containing these compounds and the use of the compounds in therapy, for example, in the treatment of diseases where under-activation of the HM74A receptor contributes to the disease or where activation of the receptor will be beneficial
Claims22
1-14. (canceled)
A compound of formula (I):
- pharmaceutically acceptable derivatives thereof,
- wherein:
- R1 represents -(alkylene)m-X-(alkylene)n-Y;
- R2 represents C1-6 alkyl, which optionally is substituted by one or more groups independently selected from cycloalkyl, C1-6 haloalkyl, halogen, —CN or —OR4;
- R3 represents halogen;
- wherein:
- m and n is number of carbon atoms in the alkylene chain;
- X is a group selected from heteroaryl or heterocyclyl;
- Y is a group selected from aryl, heteroaryl and O-aryl;
- which optionally is substituted by one or more groups independently selected from C1-6 alkyl, C2-6alkenyl, C2-6alkynyl, halogen, —(CH2)qNR5R7, —(CH2)q—(O)p—(CH2)q—N(R5)C(O)OR8, —(CH2)q—N(R5)C(O)R8, —(CH2)q—(O)p—(CH2)q—C(O)NR5R6, —(CH2)q—N(R5)C(O)NR5R6, —(CH2)q—C(O)N((CH2)mOH)R5, —(CH2)q—N(R5)—S(O)2R8, —CH2—S(O)2NR5R6, —C1-6 haloalkyl, —OCF3, —OCH(F)2, —OCH2F, —C(O)OR5, —OR5, —R8CN, CN, —SO2R9, —(CH2)nheteroaryl, —(CH2)nheterocyclyl, —(CH2)ncycloalkyl, —(CH2)ncycloalkenyl, or —(CH2)naryl;
- R4 represents a group selected from hydrogen, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, —(CH2)n cycloalkyl, —(CH2)n cycloalkenyl, —(CH2)n heterocyclyl, —(CH2)n aryl, or —(CH2)n heteroaryl;
- R5 and R6 are independently selected from hydrogen or C1-4 alkyl;
- R7 represents a group selected from C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl,
- —(CH2)t cycloalkyl, —(CH2)n cycloalkenyl, —(CH2)t heterocyclyl, —(CH2)t aryl, or —(CH2)t heteroaryl;
- R8 represents C1-4 alkyl;
- R9 represents a group selected from C1-6 alkyl C2-6 alkenyl, C2-6 alkynyl, —(CH2)n cycloalkyl, —(CH2)ncycloalkenyl, —(CH2)nheterocyclyl, —(CH2)n aryl, —(CH2)nheteroaryl, or CN;
- m represents an integer selected from 3 and 4;
- n represents an integer selected from 0 and 1;
- p represents an integer selected from 0 and 1;
- q represents an integer selected from 0, 1 and 2;
- and
- t represents an integer selected from 1 and 2.
19 more elements
Dependencies are inferred from the claim text.